RU2010126050A - ANTIBACTERIAL NUCLEOSIDE COMPOUNDS - Google Patents
ANTIBACTERIAL NUCLEOSIDE COMPOUNDS Download PDFInfo
- Publication number
- RU2010126050A RU2010126050A RU2010126050/04A RU2010126050A RU2010126050A RU 2010126050 A RU2010126050 A RU 2010126050A RU 2010126050/04 A RU2010126050/04 A RU 2010126050/04A RU 2010126050 A RU2010126050 A RU 2010126050A RU 2010126050 A RU2010126050 A RU 2010126050A
- Authority
- RU
- Russia
- Prior art keywords
- azido
- dioxaphosphorinan
- oxo
- cis
- uridine
- Prior art date
Links
- 0 B[C@@]1O[C@](*)(COP(OCC2)(OC2I)=O)CC1OC(O)=O Chemical compound B[C@@]1O[C@](*)(COP(OCC2)(OC2I)=O)CC1OC(O)=O 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/06—Pyrimidine radicals
- C07H19/10—Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/16—Purine radicals
- C07H19/20—Purine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biotechnology (AREA)
- Biochemistry (AREA)
- Oncology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Immunology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
1. Соединение общей формулы I или II ! ! в которой V обозначает фенил или пиридинил, указанный фенил или пиридинил необязательно содержит от 1 до 3 заместителей, выбранных из группы, включающей галоген, C1-C6-алкил, C1-C6-галогеналкил, C1-C6-алкоксигруппу или цианогруппу; ! B обозначает ! , или ! R1 и R2 независимо выбраны из группы, включающей H и/или COR4; ! Y обозначает O или NH; ! R3 обозначает C1-C6-алкил или COR4 и ! R4 обозначает C1-C6-алкил, C1-C3-алкокси-C1-C6-алкил, C3-C6-циклоалкил, С3-C6-циклоалкил-C1-С3-алкил, C1-C6-алкоксигруппу или гетероарил, где гетероарил представляет собой 5-членное кольцо, содержащее 1 или 2 гетероатома, выбранных из азота, кислорода и серы, или пиридин, или 6-членное кольцо, содержащее 1 или 2 атома азота; или ! его фармацевтически приемлемая соль. ! 2. Соединение формулы I по п.1, в которой B обозначает B-1. ! 3. Соединение по п.2, в котором V обозначает необязательно замещенный фенил, R1 и R2 независимо обозначают водород или COR4; и R4 обозначает C1-C6-алкил. ! 4. Соединение формулы II по п.1. ! 5. Соединение формулы II по п.3, в которой V обозначает необязательно замещенный фенил и В обозначает B-1. ! 6. Соединение по п.1, в котором В обозначает B-2. ! 7. Соединение по п.6, в котором V обозначает необязательно замещенный фенил. ! 8. Соединение по п.1, в котором B обозначает B-3. ! 9. Соединение по п.8, в котором V обозначает необязательно замещенный фенил. ! 10. Соединение по п.1, выбранное из группы, включающей: ! 4'-азидо-цис-5'-O-[4-(R,S)-(3-фторфенил)-2-оксо-1,3,2-диоксафосфоринан-2-ил]уридин; !4'-азидо-цис-5'-O-[4-(R,S)-(3-бромфенил)-2-оксо-1,3,2-диоксафосфоринан-2-ил]уридин; ! 4'-азидо-цис-5'-O-[4-(R,S)-(3-бром-4-фторфенил)-2-оксо-1,3,2-диоксафосфоринан-2-ил]уридин; ! 4'-азидо-цис-5'-O-[4-(R,S)-(3-хлор-4-фторфенил)-2-окс 1. The compound of General formula I or II! ! in which V is phenyl or pyridinyl, said phenyl or pyridinyl optionally contains from 1 to 3 substituents selected from the group consisting of halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy or cyano; ! B stands for! , or ! R1 and R2 are independently selected from the group consisting of H and / or COR4; ! Y is O or NH; ! R3 is C1-C6 alkyl or COR4 and! R4 is C1-C6-alkyl, C1-C3-alkoxy-C1-C6-alkyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C3-alkyl, C1-C6-alkoxy or heteroaryl, where heteroaryl is A 5-membered ring containing 1 or 2 heteroatoms selected from nitrogen, oxygen and sulfur, or pyridine, or a 6-membered ring containing 1 or 2 nitrogen atoms; or ! its pharmaceutically acceptable salt. ! 2. The compound of formula I according to claim 1, in which B is B-1. ! 3. The compound according to claim 2, in which V is optionally substituted phenyl, R1 and R2 are independently hydrogen or COR4; and R4 is C1-C6 alkyl. ! 4. The compound of formula II according to claim 1. ! 5. The compound of formula II according to claim 3, in which V is optionally substituted phenyl and B is B-1. ! 6. The compound according to claim 1, in which b is B-2. ! 7. The compound according to claim 6, in which V denotes optionally substituted phenyl. ! 8. The compound according to claim 1, in which B is B-3. ! 9. The compound of claim 8, in which V denotes optionally substituted phenyl. ! 10. The compound according to claim 1, selected from the group including:! 4'-azido-cis-5'-O- [4- (R, S) - (3-fluorophenyl) -2-oxo-1,3,2-dioxaphosphorinan-2-yl] uridine; ! 4'-azido-cis-5'-O- [4- (R, S) - (3-bromophenyl) -2-oxo-1,3,2-dioxaphosphorinan-2-yl] uridine; ! 4'-azido-cis-5'-O- [4- (R, S) - (3-bromo-4-fluorophenyl) -2-oxo-1,3,2-dioxaphosphorinan-2-yl] uridine; ! 4'-azido-cis-5'-O- [4- (R, S) - (3-chloro-4-fluorophenyl) -2-ox
Claims (20)
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US99116307P | 2007-11-29 | 2007-11-29 | |
US60/991,163 | 2007-11-29 | ||
US8454408P | 2008-07-29 | 2008-07-29 | |
US61/084,544 | 2008-07-29 |
Publications (1)
Publication Number | Publication Date |
---|---|
RU2010126050A true RU2010126050A (en) | 2012-01-10 |
Family
ID=40679083
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU2010126050/04A RU2010126050A (en) | 2007-11-29 | 2008-11-27 | ANTIBACTERIAL NUCLEOSIDE COMPOUNDS |
Country Status (20)
Country | Link |
---|---|
US (2) | US8063025B2 (en) |
EP (1) | EP2227481A4 (en) |
JP (1) | JP2011505351A (en) |
KR (1) | KR20100103793A (en) |
CN (1) | CN102164939A (en) |
AR (1) | AR069740A1 (en) |
AU (1) | AU2008331158A1 (en) |
BR (1) | BRPI0819797A2 (en) |
CA (1) | CA2706432A1 (en) |
CL (1) | CL2008003511A1 (en) |
CO (1) | CO6382185A2 (en) |
CR (1) | CR11453A (en) |
EC (1) | ECSP10010210A (en) |
IL (1) | IL205625A0 (en) |
MA (1) | MA31864B1 (en) |
MX (1) | MX2010005885A (en) |
RU (1) | RU2010126050A (en) |
TW (1) | TW200936146A (en) |
WO (1) | WO2009069095A2 (en) |
ZA (1) | ZA201003438B (en) |
Families Citing this family (19)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
BRPI0819831A2 (en) | 2007-11-29 | 2019-09-24 | Boehringer Ingelheim Int | 6,7-dihydro-5h-imidazo [1,2-a] imidazole-3-carboxylic acid amide derivatives |
TW201141488A (en) * | 2010-01-28 | 2011-12-01 | Hoffmann La Roche | Antiviral nucleosides |
AU2011305652B2 (en) | 2010-09-22 | 2016-10-20 | Janssen Biopharma, Inc. | Azido nucleosides and nucleotide analogs |
JP6069215B2 (en) | 2010-11-30 | 2017-02-01 | ギリアド ファーマセット エルエルシー | Compound |
EP2776438A4 (en) * | 2011-11-10 | 2015-04-29 | Inhibitex Inc | Substituted purine nucleosides, phosphoramidate and phosphordiamidate derivatives for treatment of viral infections |
US9676809B2 (en) | 2013-11-22 | 2017-06-13 | Ligand Pharmaceuticals Incorporated | Derivatives of uridine 5′-cyclophosphate useful to treat hepatitis C viral infections |
CN103848877B (en) * | 2013-12-16 | 2016-08-24 | 安徽贝克联合制药有限公司 | Nucleoside cyclic phosphate compound and preparation method thereof and its application |
US10449210B2 (en) | 2014-02-13 | 2019-10-22 | Ligand Pharmaceuticals Inc. | Prodrug compounds and their uses |
EP3164136A4 (en) | 2014-07-02 | 2018-04-04 | Ligand Pharmaceuticals, Inc. | Prodrug compounds and uses therof |
WO2017024255A1 (en) | 2015-08-05 | 2017-02-09 | Metrobiotech, Llc | Nicotinamide mononucleotide derivatives and their uses |
WO2018129040A1 (en) | 2017-01-04 | 2018-07-12 | President And Fellows Of Harvard College | Modulating nudix homology domain (nhd) with nicotinamide mononucleotide analogs and derivatives of same |
CN108727450B (en) * | 2017-04-18 | 2024-02-20 | 浙江柏拉阿图医药科技有限公司 | Liver delivery anti-hepatitis C prodrug nucleoside cyclic phosphate compound and application thereof |
CN109956986B (en) * | 2017-12-22 | 2021-04-27 | 浙江柏拉阿图医药科技有限公司 | Liver delivery gemcitabine prodrug nucleoside cyclic phosphate compound and application thereof |
CN109956975B (en) * | 2017-12-22 | 2020-11-06 | 浙江柏拉阿图医药科技有限公司 | Liver delivery entecavir prodrug nucleoside cyclic phosphate ester compound and application thereof |
CN109956985A (en) * | 2017-12-22 | 2019-07-02 | 浙江柏拉阿图医药科技有限公司 | Liver delivers cytarabine pro-drug nucleosides cyclic phosphate compound and application |
RU2020126177A (en) | 2018-01-09 | 2022-02-10 | Лиганд Фармасьютикалз, Инк. | ACETAL COMPOUNDS AND THEIR THERAPEUTIC APPLICATIONS |
CN111434671B (en) * | 2019-01-11 | 2023-07-11 | 凯思凯迪(上海)医药科技有限公司 | Liver-specific AMPK agonist and preparation method and application thereof |
TW202322824A (en) | 2020-02-18 | 2023-06-16 | 美商基利科學股份有限公司 | Antiviral compounds |
WO2022221514A1 (en) | 2021-04-16 | 2022-10-20 | Gilead Sciences, Inc. | Methods of preparing carbanucleosides using amides |
Family Cites Families (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU767599B2 (en) * | 1998-03-06 | 2003-11-20 | Metabasis Therapeutics, Inc. | Novel prodrugs for phosphorus-containing compounds |
GB0114286D0 (en) * | 2001-06-12 | 2001-08-01 | Hoffmann La Roche | Nucleoside Derivatives |
KR101115210B1 (en) | 2002-10-31 | 2012-04-12 | 메타베이시스 테라퓨틱스, 인크. | Novel cytarabine monophosphate prodrugs |
TWI332507B (en) * | 2002-11-19 | 2010-11-01 | Hoffmann La Roche | Antiviral nucleoside derivatives |
ATE478886T1 (en) | 2003-07-25 | 2010-09-15 | Idenix Pharmaceuticals Inc | PURINE NUCLEOSIDES FOR THE TREATMENT OF DISEASES CAUSED BY FLAVIVIDRAE, INCLUDING HEPATITIS C |
EP1781101A2 (en) | 2004-07-29 | 2007-05-09 | Metabasis Therapeutics, Inc. | Novel nucleoside derivatives |
CA2618335C (en) * | 2005-08-15 | 2015-03-31 | F.Hoffmann-La Roche Ag | Antiviral phosphoramidates of 4'-substituted pronucleotides |
JP4954573B2 (en) * | 2006-02-28 | 2012-06-20 | オリンパス株式会社 | Endoscope system |
-
2008
- 2008-11-26 CL CL2008003511A patent/CL2008003511A1/en unknown
- 2008-11-26 US US12/313,992 patent/US8063025B2/en active Active
- 2008-11-26 AR ARP080105126A patent/AR069740A1/en not_active Application Discontinuation
- 2008-11-26 TW TW097145866A patent/TW200936146A/en unknown
- 2008-11-27 AU AU2008331158A patent/AU2008331158A1/en not_active Abandoned
- 2008-11-27 KR KR1020107011589A patent/KR20100103793A/en not_active Application Discontinuation
- 2008-11-27 JP JP2010535494A patent/JP2011505351A/en active Pending
- 2008-11-27 CA CA2706432A patent/CA2706432A1/en not_active Abandoned
- 2008-11-27 EP EP08855731A patent/EP2227481A4/en not_active Withdrawn
- 2008-11-27 MX MX2010005885A patent/MX2010005885A/en not_active Application Discontinuation
- 2008-11-27 WO PCT/IB2008/054985 patent/WO2009069095A2/en active Application Filing
- 2008-11-27 RU RU2010126050/04A patent/RU2010126050A/en not_active Application Discontinuation
- 2008-11-27 CN CN2008801185991A patent/CN102164939A/en active Pending
- 2008-11-27 BR BRPI0819797A patent/BRPI0819797A2/en not_active IP Right Cessation
-
2010
- 2010-05-09 IL IL205625A patent/IL205625A0/en unknown
- 2010-05-13 CO CO10057513A patent/CO6382185A2/en not_active Application Discontinuation
- 2010-05-14 ZA ZA2010/03438A patent/ZA201003438B/en unknown
- 2010-05-21 CR CR11453A patent/CR11453A/en not_active Application Discontinuation
- 2010-05-27 MA MA32870A patent/MA31864B1/en unknown
- 2010-05-28 EC EC2010010210A patent/ECSP10010210A/en unknown
-
2011
- 2011-10-26 US US13/282,100 patent/US20120039845A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
AU2008331158A1 (en) | 2009-06-04 |
JP2011505351A (en) | 2011-02-24 |
KR20100103793A (en) | 2010-09-28 |
EP2227481A4 (en) | 2011-03-09 |
CR11453A (en) | 2010-10-27 |
US20120039845A1 (en) | 2012-02-16 |
WO2009069095A2 (en) | 2009-06-04 |
MX2010005885A (en) | 2010-11-24 |
IL205625A0 (en) | 2010-11-30 |
AR069740A1 (en) | 2010-02-17 |
TW200936146A (en) | 2009-09-01 |
CO6382185A2 (en) | 2012-02-15 |
ZA201003438B (en) | 2011-04-28 |
MA31864B1 (en) | 2010-11-01 |
US8063025B2 (en) | 2011-11-22 |
EP2227481A2 (en) | 2010-09-15 |
US20090209481A1 (en) | 2009-08-20 |
CA2706432A1 (en) | 2009-06-04 |
CL2008003511A1 (en) | 2010-02-19 |
CN102164939A (en) | 2011-08-24 |
ECSP10010210A (en) | 2010-08-31 |
BRPI0819797A2 (en) | 2019-09-24 |
WO2009069095A3 (en) | 2009-12-23 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20120412 |